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    GSK8612
    GSK8612

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V4435
    CAS #: 2361659-62-1Purity ≥98%

    Description: GSK8612 is a novel, potent and highly selective small molecule inhibitor of Tank-binding Kinase-1 (TBK1) with a pIC50 of 6.8 for recombinant TBK1. The serine/threonine protein kinase TBK1 (Tank-binding Kinase-1) is a noncanonical member of the IkB kinase (IKK) family. This kinase regulates signaling pathways in innate immunity, oncogenesis, energy homeostasis, autophagy, and neuroinflammation. In cellular assays, GSK861 inhibited toll-like receptor (TLR)3-induced interferon regulatory factor (IRF)3 phosphorylation in Ramos cells and type I interferon (IFN) secretion in primary human mononuclear cells. In THP1 cells, GSK8612 was able to inhibit secretion of interferon beta (IFNβ) in response to dsDNA and cGAMP, the natural ligand for STING. GSK8612 is a TBK1 small molecule inhibitor displaying an excellent selectivity profile and therefore represents an ideal probe to further dissect the biology of TBK1 in models of immunity, neuroinflammation, obesity, or cancer.

    References: ACS Med Chem Lett. 2019 Mar 11;10(5):780-785.


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    GSK8612

    Name: GSK8612
    CAS#: 2361659-62-1
    Chemical Formula: C17H17BrF3N7O2S
    Exact Mass: 519.03
    Molecular Weight: 520.3292
    Elemental Analysis: C, 39.24; H, 3.29; Br, 15.36; F, 10.95; N, 18.84; O, 6.15; S, 6.16
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Technical InformationSynonym: GSK-8612; GSK 8612; GSK8612;
    Chemical Name: 4-((5-bromo-2-((3-methyl-1-(2,2,2-trifluoroethyl)-1H-pyrazol-4-yl)amino)pyrimidin-4-ylamino)methyl)benzenesulfonamide
    SMILES Code: O=S(C1=CC=C(CNC2=NC(NC3=CN(CC(F)(F)F)N=C3C)=NC=C2Br)C=C1)(N)=O


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     GSK8612


    ACS Med Chem Lett. 2019 Mar 11;10(5):780-785.




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